1. Gold(I)-mediated inhibition of protein tyrosine phosphatases: a detailed in vitro and cellular study.
- Author
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Krishnamurthy D, Karver MR, Fiorillo E, Orrú V, Stanford SM, Bottini N, and Barrios AM
- Subjects
- Cell Line, Enzyme Inhibitors chemistry, Gold Compounds chemistry, Humans, Hydrogen-Ion Concentration, Molecular Structure, Protein Tyrosine Phosphatases metabolism, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Gold Compounds chemical synthesis, Gold Compounds pharmacology, Protein Tyrosine Phosphatases antagonists & inhibitors
- Abstract
Gold(I) complexes containing N-heterocyclic carbene ligands were synthesized, characterized, and along with the antiarthritic drug, auranofin, tested as inhibitors of the cysteine-dependent protein tyrosine phosphatases, which are implicated in several disease states. These compounds exhibit potencies in the low micromolar range against the enzymes in vitro. At therapeutically relevant concentrations, all compounds inhibit PTP activity in Jurkat T leukemia cells with some selectivity. In addition, the gold-carbene compounds inhibit phosphatase activity in primary mouse thymocytes.
- Published
- 2008
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